Abstract
The two reported metabotropic glutamate receptor (mGluR) antagonists, α-methyl-cyclopropyl glycine (MCCG) and α-methyl-aminophosphonobutyrate (MAP4) were tested on the mGluR1b, mGluR2 and mGluR4a subtypes of human mGluRs. Neither MCCG (500 μM) nor MAP4 (500 μM) antagonized the activation of mGluR1b by 10 μM quisqualate. MCCG was found to potently antagonize the action of 30 μM (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid [(1S,3R)-ACPD] at mGluR2 (IC50 = 87.5 μM; apparent KD = 25 μM) but did not block the action of 1 μM S-2-amino-4-phosphonobutyric acid at mGluR4a (IC50 > 1 mM). MAP4 was found to be a weak antagonist or partial agonist at mGluR4a (IC50 > 500 μM) and, less potently, also antagonized the action of 30 μM (1S,3R)-ACPD) at mGluR2 (IC50 ~2 mM).
Original language | English |
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Pages (from-to) | 1099-1102 |
Number of pages | 4 |
Journal | Neuropharmacology |
Volume | 34 |
Issue number | 8 |
DOIs | |
Publication status | Published - Aug 1995 |
User-Defined Keywords
- (1S,3R)-ACPD
- antagonism
- L-AP4
- Recombinant receptors
- α-methyl-amino acids